It seems that both naringin and hesperidin are anti-inflammatory and antioxidative in nature, but hesperidin proved to be better than indomethacin and naringin because of more pronounced pharmacological actions without tissue toxicity.

Peel extracts from Citrus sinensis, Punica granatum, and Musa paradisiaca were investigated for their effects on tissue lipid peroxidation (LPO) and on the concentration of thyroid hormones, insulin, and glucose in male rats. In vitro inhibition of H(2)O(2)-induced LPO in red blood cells of rats by 0.25, 0.50, 1.0, and 2.0 microg/mL C. sinensis, P. granatum, and M. paradisiaca peel extracts was observed in a dose-specific manner. Maximum inhibition was observed at 0.50 microg/mL C. sinensis, 2.0 microg/mL P. granatum, and 1.0 microg/mL M. paradisiaca. In the in vivo investigation, out of four different concentrations of each peel extract, 25, 200, and 100 mg/kg C. sinensis, P. granatum, and M. paradisiaca, respectively, were found to maximally inhibit hepatic LPO. The most effective doses were further evaluated for effects on serum triiodothyronine (T(3)), thyroxine (T(4)), insulin, and glucose concentrations. C. sinensis exhibited antithyroidal, hypoglycemic, and insulin stimulatory activities, in addition to inhibition of LPO, as it significantly decreased the serum T(4) (P < .05) and glucose (P < .001) concentrations with a concomitant increase in insulin levels (P < .05). P. granatum decreased LPO in hepatic, cardiac, and renal tissues (P < .01, P < .001, and P < .05, respectively) and serum glucose concentration (P < .01). M. paradisiaca strongly inhibited the serum level of thyroid hormones (P < .01 for both T(3) and T(4)) but increased the level of glucose (P < .05). These findings reveal the hitherto unknown potential of the tested peel extracts in the regulation of thyroid function and glucose metabolism. Besides antiperoxidative activity, C. sinensis extract has antithyroidal, hypoglycemic, and insulin stimulatory properties, which suggest its potential to ameliorate both hyperthyroidism and diabetes mellitus.

Here, we report the self-assembly of Amoc (9-anthracenemethoxycarbonyl)-capped dipeptides, which self-assemble to form injectable, self-healable, and shape-memory hydrogels with inherent antibacterial properties. Amoc-capped dipeptides self-assemble to form nanofibrillar networks, which are established by several spectroscopic and microscopic techniques. The inherent antibacterial properties of hydrogels are evaluated using two Gram-positive Staphylococcus aureus, Bacillus subtilis and three Gram-negative Escherichia coli, Pseudomonas aeruginosa, and Salmonella typhi bacteria. These hydrogels exhibit potent antibacterial efficacy against Gram-positive and Gram-negative bacteria. The minimum inhibitory concentrations (MIC) for the hydrogels on Gram-positive bacteria are in the range of 10-200 μM hydrogelator concentrations. The biocompatibility and cytotoxicity of the hydrogels are evaluated using 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT), hemolysis, and lipid peroxidation (LPO) assay on human blood cells. The hydrogels are hemocompatible and they decrease LPO values on human red blood cells probably via increased cellular stability against oxidative stress. Furthermore, MTT data show that the hydrogels are biocompatible and promote cell viability and proliferation on cultured human white blood cells. Taken together, these results may suggest that our designed injectable hydrogels could be useful to prevent localized bacterial infections.

An investigation on the effects of four different concentrations of peel extract from Citrus sinensis (CS) or Punica granatum (PG) in male mice revealed the maximum glucose lowering and antiperoxidative activities at 25 mg/kg of CS and 200 mg/kg of PG. In a separate experiment their potential was evaluated with respect to the regulation of alloxan induced diabetes mellitus. While a single dose of alloxan (120 mg/kg) increased the serum levels of glucose and alpha-amylase activity, rate of water consumption and lipid peroxidation (LPO) in hepatic, cardiac and renal tissues with a parallel decrease in serum insulin level, administration of 25 mg/kg of CS or 200 mg/kg of PG was found to normalize all the adverse changes induced by alloxan, revealing the antidiabetic and anti peroxidative potential of test fruit peel extracts. Subsequent phytochemical analysis indicated that the high content of total polyphenols in the test peels might be related to the antidiabetic and antiperoxidative effects of the test peels.

The development of a peptide-based coassembled thixotropic hydrogel is a promising biomaterial, which could be used for dermal wound healing application. Cyclodextrins are widely used as biocompatible cyclic oligosaccharides that have hydrophilic exterior and hydrophobic interior for the formation of functional biomaterials. The current work presents a paradigm of a coassembled hydrogel with suitable mechanical strength that exhibits in vivo wound healing efficacy. In this report, we have designed and synthesized an Amoc (9-anthracenemethoxycarbonyl)-capped dipeptide, which self-assembles into a tough and robust hydrogel owing to participation of various noncovalent interactions. The mechanical strength of the self-assembling peptide-based hydrogel is tuned by incorporation of equimolar β-cyclodextrin (CD), which leads to the formation of a coassembled hydrogel suitable for wound healing application. The coassembled hydrogel exhibits simple syringe injectability and is thixotropic in nature. The nanostructural morphology of the coassembled hydrogel reveals a highly cross-linked and entangled nanofibrillar network. Several spectroscopic data elucidate the presence of noncovalent interactions between CD and peptide, which could be the driving force for the formation of ordered nanostructures. The coassembled hydrogel shows potent antibacterial activity against Gram-positive pathogenic bacteria. In vitro biocompatibility of the coassembled hydrogel has been investigated with the human embryonic kidney (HEK293) and MCF-7 cell lines. Additionally, confocal laser scanning microscopic data show cellular uptake of the coassembled hydrogel with blue fluorescence. Moreover, the in vivo wound healing activity of the coassembled hydrogel has been investigated by the histopathology study. The biochemical parameters such as nitric oxide and collagen contents have been evaluated by Griess and hydroxy proline assays. All the results corroborate the wound healing efficacy of a nanofibrillar antibacterial coassembled hydrogel.

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We report lipase-catalyzed inclusion of p-hydroxy benzylalcohol to peptide bolaamphiphiles. The lipase-catalyzed reactions of peptide bolaamphiphiles with p-hydroxy benzylalcohol generate dynamic combinatorial libraries (DCL) in aqueous medium that mimic the natural dissipative system. The peptide bolaamphiphile 1 (HO-WY-Suc-YW-OH) reacts with p-hydroxy benzylalcohol in the presence of lipase forming an activated diester building block. The activated diester building block self-assembles to produce nanofibrillar thixotropic hydrogel. The subsequent hydrolysis results in the dissipation of energy to form nonassembling bolaamphiphile 1 with collapsed nanofibers. The thixotropic DCL hydrogel matrix is used for 3D cell culture experiments for different periods of time, significantly supporting the cell survival and proliferation of human umbilical cord mesenchymal stem cells.